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Assay Detail

CHEMBL2154121

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human OCT2 A270S mutant expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
Kido Y, Matsson P, Giacomini KM.
J Med Chem (2011) 54 : 4548 -4558
PubMed 21599003 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.44 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 5.92
CHEMBL11 IMIPRAMINE 4.0 1 5.68
CHEMBL46 ONDANSETRON 4.0 1 5.55
CHEMBL932 DIPYRIDAMOLE 4.0 1 5.42
CHEMBL517 DISOPYRAMIDE 4.0 1 5.41
CHEMBL900 ORPHENADRINE 4.0 1 5.37
CHEMBL30 CIMETIDINE 4.0 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 1200.0 nM 5.92
CHEMBL11 IMIPRAMINE IC50 = 2100.0 nM 5.68
CHEMBL46 ONDANSETRON IC50 = 2800.0 nM 5.55
CHEMBL932 DIPYRIDAMOLE IC50 = 3800.0 nM 5.42
CHEMBL517 DISOPYRAMIDE IC50 = 3900.0 nM 5.41
CHEMBL900 ORPHENADRINE IC50 = 4300.0 nM 5.37
CHEMBL30 CIMETIDINE IC50 = 20000.0 nM 4.70